URSO (Tablet, Film Coated)

URSO (Tablet, Film Coated)

Ursodiol (UDCA) is normally present as a minor fraction of the total bile acids in humans (about 5%). Following oral administration, the majority of ursodiol is absorbed by passive diffusion and its absorption is incomplete. Once absorbed, ursodiol undergoes hepatic extraction to the extent of about 50% in the absence of liver disease. As the severity of liver disease increases, the extent of extraction decreases. In the liver, ursodiol is conjugated with glycine or taurine, then secreted into bile. These conjugates of ursodiol are absorbed in the small intestine by passive and active mechanisms. The conjugates can also be deconjugated in the ileum by intestinal enzymes, leading to the formation of free ursodiol that can be reabsorbed and reconjugated in the liver. Nonabsorbed ursodiol passes into the colon where it is mostly 7-dehydroxylated to lithocholic acid. Some ursodiol is epimerized to chenodiol (CDCA) via a 7-oxo intermediate. Chenodiol also undergoes 7-dehydroxylation to form lithocholic acid. These metabolites are poorly soluble and excreted in the feces. A small portion of lithocholic acid is reabsorbed, conjugated in the liver with glycine, or taurine and sulfated at the 3 position. The resulting sulfated lithocholic acid conjugates are excreted in bile and then lost in feces. Lithocholic acid, when administered chronically to animals, causes cholestatic liver injury that may lead to death from liver failure in certain species unable to form sulfate conjugates. Ursodiol is 7-dehydroxylated more slowly than chenodiol. For equimolar doses of ursodiol and chenodiol, steady state levels of lithocholic acid in biliary bile acids are lower during ursodiol administration than with chenodiol administration. Humans and chimpanzeescan sulfate lithocholic acid. Although liver injury has not been associated with ursodiol therapy, a reduced capacity to sulfate may exist in some individuals. Nonetheless, such a deficiency has not yet been clearly demonstrated and must be extremely rare, given the several thousand patient-years of clinical experience with ursodiol. In healthy subjects, at least 70% of ursodiol (unconjugated) is bound to plasma protein. No information is available on the binding of conjugated ursodiol to plasma protein in healthy subjects or primary biliary cirrhosis (PBC) patients. Its volume of distribution has not been determined, but is expected to be small since the drug is mostly distributed in the bile and small intestine. Ursodiol is excreted primarily in the feces. With treatment, urinary excretion increases, but remains less than 1% except in severe cholestatic liver disease. During chronic administration of ursodiol, it becomes a major biliary and plasma bile acid. At a chronic dose of 13 to 15 mg/kg/day, ursodiol constitutes 30-50% of biliary and plasma bile acids.

Each URSO 250 elliptical, biconvex, film-coated tablet, white, engraved with "URS785", contains 250 mg of ursodiol. Available in bottles of 100 tablets (NDC 58914-785-10) and 500 tablets (NDC 58914-785-50). Each URSO Forte elliptical, biconvex, scored, film-coated tablet, white, engraved with "URS790", contains 500 mg of ursodiol. Available in bottles of 100 tablets (NDC 58914-790-10) and 500 tablets (NDC 58914-790-50). Store at 20C to 25C (68F to 77F). Dispense in a tight container. Manufactured in Canada for:Axcan Scandipharm Inc.22 Inverness Center ParkwayBirmingham, AL 35242USAwww.axcan.com URSO 250 and URSO Forte are registered trademarks used under license by Axcan Scandipharm Inc.Revision date: March 10, 2008Printed in Canada.

dailymed-ingredient:carnauba_wax, dailymed-ingredient:cetyl_alcohol, dailymed-ingredient:dibutyl_sebacate, dailymed-ingredient:ethylcellulose, dailymed-ingredient:hydrogen_peroxide, dailymed-ingredient:hydroxypropyl_methylcellulose_2910, dailymed-ingredient:magnesium_stearate, dailymed-ingredient:microcrystalline_cellulose, dailymed-ingredient:polyethylene_glycol_3350, dailymed-ingredient:polyethylene_glycol_8000, dailymed-ingredient:povidone, dailymed-ingredient:sodium_lauryl_sulfate, dailymed-ingredient:sodium_starch_glycolate

URSO (Tablet, Film Coated)

http://www4.wiwiss.fu-berlin.de/dailymed/resource/organization/Axcan_Scandipharm_Inc.

URSO